General description
一种与拉曲匹定(DMEBON)有关的药物,它具有神经保护和促神经原作用。
P7C3 is a drug related to latrepirdine (dimebon), which has neuroprotective and proneurogenic effects, and may be potentially useful for the treatment of Alzheimer's disease and similar neurodegenerative disorders. The precise mechanism of action through which these effects are exerted remains unclear as of 2010, but the pharmacological effects of P7C3 in vitro resemble those of endogenous proneurogenic peptides such as fibroblast growth factor 1, and the proneurogenic activity of P7C3 was around thirty times that of dimebon when they were compared side by side in mice. P7C3 was chosen for further animal studies on the basis of favourable pharmacokinetic factors, such as its high oral bioavailability and long duration of action, but several other related compounds showed similar activity such as the more potent fluorinated analogue P7C3A20 which is up to ten times stronger again, and the methoxy analogue P7C3-OMe, for which it was determined that the (R) enantiomer is the active form.
P7C3是与latrepirdine(dimebon)有关的药物,具有神经保护和促神经原作用,可能潜在地用于治疗阿尔茨海默氏病和类似的神经退行性疾病。 截至2010年,发挥这些作用的确切作用机理仍不清楚,但P7C3的体外药理作用类似于内源性神经原性肽(如成纤维细胞生长因子1)的药理作用,P7C3的神经原性活性约为其的30倍。 当它们在小鼠中并排比较时,它们的药效很差。 基于良好的药代动力学因素(例如口服生物利用度高和作用持续时间长),P7C3被选择用于进一步的动物研究,但是其他几种相关化合物也表现出相似的活性,例如更强的氟化类似物P7C3A20,其强度高达十倍。 再次确定甲氧基类似物P7C3-OMe,对于该甲氧基类似物,确定(R)对映异构体为活性形式。
Properties
Iupac Name: | N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-3-methoxyaniline |
Inchi Code | 1S/C22H19Br2FN2O/c1-28-18-4-2-3-17(11-18)26-12-16(25)13-27-21-7-5-14(23)9-19(21)20-10-15(24)6-8-22(20)27/h2-11,16,26H,12-13H2,1H3 |
Inchi Key | XNLTWMQBJFWQOU-UHFFFAOYSA-N |
安全信息